反应详情

A mixture of 5-Chloro-7-(6-methoxy-pyridin-3-yl)-[1,2,4]triazolo[1,5-a]pyridin-2-ylamine, which may be produced similar to Example 1A but substituting 6-methoxy-pyridine-3-boronic acid for 3-pyridine boronic acid (300 mg, 1.09 mmol), 2-methyl-oxazole (450 mg, 5.4 mmol), [Pd(PPh3)4] (130 mg, 0.11 mmol), KOAc (534 mg, 5.45 mmol) and DMA (4 mL) was microwaved at 200° C. for 15 min. The cooled mixture was taken up in MeOH/CHCl3, filtered through Celite, and then the filtrate was pre-adsorbed on SiO2. Column chromatography (3% MeOH/CHCl3) gave a solid which was triturated with a 1:1 mixture of DCM/hexane. Filtration gave 7-(6-methoxy-pyridin-3-yl)-5-(2-methyl-oxazol-5-yl)-[1,2,4]triazolo[1,5-a]pyridin-2-ylamine.

1. custommay be produced similar to Example 1A
2. customwas microwaved at 200° C. for 15 min
3. filtrationfiltered through Celite
4. customColumn chromatography (3% MeOH/CHCl3) gave a solid which
5. customwas triturated with a 1:1 mixture of DCM/hexane
6. filtrationFiltration